[HTML][HTML] Medicinal attributes of pyrazolo [1, 5-a] pyrimidine based scaffold derivatives targeting kinases as anticancer agents
NSM Ismail, GME Ali, DA Ibrahim… - Future Journal of …, 2016 - Elsevier
Pyrazolo pyrimidines are fused heterocyclic ring systems which known as bioisosteres of
adenine, that are necessary for every aspect of cell life. Pyrazolo [1, 5-a] pyrimidines …
adenine, that are necessary for every aspect of cell life. Pyrazolo [1, 5-a] pyrimidines …
Small molecule CDK inhibitors for the therapeutic management of cancer
Cyclin-dependent kinases (CDKs) are a group of multifunctional enzymes consisting of
catalytic and regulatory subunits. The regulatory subunit, cyclin, remains dissociated under …
catalytic and regulatory subunits. The regulatory subunit, cyclin, remains dissociated under …
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity
A Balbi, M Anzaldi, C Macciò, C Aiello, M Mazzei… - European journal of …, 2011 - Elsevier
We synthesized thirty-six novel pyrazole derivatives and studied their antiproliferative activity
in human ovarian adenocarcinoma A2780 cells, human lung carcinoma A549 cells, and …
in human ovarian adenocarcinoma A2780 cells, human lung carcinoma A549 cells, and …
Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent …
MG Brasca, N Amboldi, D Ballinari… - Journal of medicinal …, 2009 - ACS Publications
The discovery of a novel class of inhibitors of cyclin dependent kinases (CDKs) is described.
Starting from compound 1, showing good potency as inhibitor of CDKs but being poorly …
Starting from compound 1, showing good potency as inhibitor of CDKs but being poorly …
Design, synthesis and biological evaluation of certain CDK2 inhibitors based on pyrazole and pyrazolo [1, 5-a] pyrimidine scaffold with apoptotic activity
GME Ali, DA Ibrahim, AM Elmetwali, NSM Ismail - Bioorganic Chemistry, 2019 - Elsevier
Different series of novel pyrazole and pyrazolo [1, 5-a] pyrimidine derivatives (2a-g),(3a-
c),(7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit …
c),(7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit …
New approaches for the synthesis of pyrazole, thiophene, thieno[2,3-b]pyridine, and thiazole derivatives together with their anti-tumor evaluations
RM Mohareb, AEM Abdallah, MA Abdelaziz - Medicinal Chemistry …, 2014 - Springer
The reaction of cyanoacetylhydrazine (1) with acetylchloride (2) gave the N-acyl derivative 3.
The latter underwent ready cyclization in sodium ethoxide to give the pyrazole derivative 4 …
The latter underwent ready cyclization in sodium ethoxide to give the pyrazole derivative 4 …
Optimization of 6, 6-dimethyl pyrrolo [3, 4-c] pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing
MG Brasca, C Albanese, R Alzani, R Amici… - Bioorganic & medicinal …, 2010 - Elsevier
We have recently reported CDK inhibitors based on the 6-substituted pyrrolo [3, 4-c]
pyrazole core structure. Improvement of inhibitory potency against multiple CDKs …
pyrazole core structure. Improvement of inhibitory potency against multiple CDKs …
Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy
C Albanese, R Alzani, N Amboldi, N Avanzi… - Molecular cancer …, 2010 - AACR
Altered expression and activity of cyclin-dependent kinase (CDK) and tropomyosin receptor
kinase (TRK) families are observed in a wide variety of tumors. In those malignancies with …
kinase (TRK) families are observed in a wide variety of tumors. In those malignancies with …
Advances in pyrazole based scaffold as cyclin-dependent kinase 2 inhibitors for the treatment of cancer
The transformation of a normal cell into a tumor cell is one of the initial steps in cell cycle
deregulation. The cell cycle is regulated by cyclin-dependent kinases (CDKs) that belong to …
deregulation. The cell cycle is regulated by cyclin-dependent kinases (CDKs) that belong to …
Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors
KM Qiu, R Yan, M Xing, HH Wang, HE Cui… - Bioorganic & medicinal …, 2012 - Elsevier
A series of dihydro-pyrazolyl-thiazolinone derivatives (5a–5t) have been synthesized and
their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) …
their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) …